Combinations of Piperine with Hydroxypropyl-β-Cyclodextrin as a Multifunctional System

Piperine is an alkaloid that has extensive pharmacological activity and impacts other active substances bioavailability due to inhibition of CYP450 enzymes, stimulation of amino acid transporters and P-glycoprotein inhibition. Low solubility and the associated low bioavailability of piperine limit its potential. The combination of piperine with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) causes a significant increase in its solubility and, consequently, an increase in permeability through gastrointestinal tract membranes and the blood–brain barrier. X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR), nuclear magnetic resonance (NMR) were used to characterize interactions between piperine and HP-β-CD. The observed physicochemical changes should be combined with the process of piperine and CD system formation. Importantly, with an increase in solubility and permeability of piperine as a result of interaction with CD, it was proven to maintain its biological activity concerning the antioxidant potential (2,2-diphenyl-1-picryl-hydrazyl-hydrate assay), inhibition of enzymes essential for the inflammatory process and for neurodegenerative changes (hyaluronidase, acetylcholinesterase, butyrylcholinesterase).     

A Potent Mimetic of the Siglec-8 Ligand 6’-Sulfo-Sialyl Lewisx

Siglecs are members of the immunoglobulin gene family containing sialic acid binding N-terminal domains. Among them, Siglec-8 is expressed on various cell types of the immune system such as eosinophils, mast cells and weakly on basophils. Cross-linking of Siglec-8 with monoclonal antibodies triggers apoptosis in eosinophils and inhibits degranulation of mast cells, making Siglec-8 a promising target for the treatment of eosinophil- and mast cell-associated diseases such as asthma. The tetrasaccharide 6’-sulfo-sialyl Lewis^x has been identified as a specific Siglec-8 ligand in glycan array screening. Here, we describe an extended study enlightening the pharmacophores of 6’-sulfo-sialyl Lewis^x and the successful development of a high-affinity mimetic. Retaining the neuraminic acid core, the introduction of a carbocyclic mimetic of the Gal moiety and a sulfonamide substituent in the 9-position gave a 20-fold improved binding affinity. Finally, the residence time, which usually is the Achilles tendon of carbohydrate/lectin interactions, could be improved.     

Thermo-protective properties of polymer composites with nano-titanium dioxide

International Journal of Mechanics and Materials in Design - The present work investigates the ablative and thermal properties of an epoxy resin which was modified with titanium dioxide...     

Potential tissue implants from the networks based on 1,5-dioxepan-2-one and ε-caprolactone

The synthesis and characterization of degradable polymeric networks for biomedical applications was performed. Cross-linked films of poly(ε-caprolactone) (PCL) and poly(1,5-dioxepan-2-one) (PDXO) having various mole fractions of monomers and different cross-link densities were successfully prepared using 2,2′-bis-(ε-caprolactone-4-yl) propane (BCP) as cross-linking agent. Reaction parameters were carefully examined to optimise the film-forming conditions. Networks obtained were elastomeric materials, easy to cast and remove from the mould. Effect of CL content and cross-link density on the final properties of the polymer network was evaluated. High CL content or degree of cross-linking led to increase in Young's modulus and decrease in elongation at break. An increase in crystalline domains in films having a higher CL content was observed by optical microscopy. A greater thermal stability was observed in films having a high CL content. The hydrophilicity of the materials could be tailored by changing the CL content. The surface of the films became rougher with higher CL content.     

Inorganic–organic hybrid materials with zirconium oxoclusters as protective coatings on aluminium alloys

Inorganic–organic hybrid materials are attracting a strong scientific interest mainly for their outstanding inherent mechanical and thermal properties, which can be traced back to the intimate coupling of both inorganic and organic components. By carefully choosing the experimental parameters used for their synthesis, chemically and thermally stable acrylate-based hybrid material embedding the zirconium oxocluster Zr₄O₄(OMc)₁₂, where OMcCH₂C(CH₃)C(O)O, can be deposited as UV-cured films on aluminium alloys.

In particular, the molar ratios between the oxocluster and the monomer, the polymerisation time, the amount of photo-initiator and the deposition conditions, by using an home-made spray-coating equipment, were optimised in order to obtain the best performing layers in terms of transparency and hardness to coat aluminium alloy (AA1050, AA6060 and AA2024) sheets. Furthermore, it was also evaluated whether the hybrid coatings behave as barrier to corrosion.

Several coated samples were prepared and characterised. Environmental scanning electronic microscopy (ESEM) and scratch test were used to investigate the morphology of the films and to evaluate their scratch resistance, respectively. Electrochemical impedance spectroscopy (EIS) was performed in order to evaluate if the coatings actually protect the metallic substrate from corrosion.

In order to measure shear storage modulus (G′) and loss modulus (G″) of the materials used for coatings, bulk samples were also obtained by UV-curing of the precursors solution. Dynamical mechanical thermal analysis (DMTA) was performed in shear mode on cured disks of both the hybrid materials and pristine polymer for comparison. The values of T_g were read off as the temperatures of peak of loss modulus. The length and mass of all the samples were measured before and after the DMTA analysis, so that the shrinkage of the materials in that temperature range was exactly evaluated.     

Sensitivity analysis of the scattering parameters of microwave filters using the adjoint network method

A novel approach is presented to calculate the sensitivities of the scattering parameters of microwave filters obtained with the full‐wave mode‐matching (MM) technique. Using only the MM simulation of the original network, the sensitivities of the scattering parameters with respect to all designable parameters are obtained. The adjoint network method (ANM) is applied to the generalized scattering matrices of the different filter components. This guarantees good accuracy of the calculated sensitivities. The implementation details are discussed for N‐resonator ridge waveguide filters. Excellent agreement is obtained between the sensitivities calculated using ANM and those obtained using the expensive central differences. © 2006 Wiley Periodicals, Inc. Int J RF and Microwave CAE, 2006.     

Glyconanoparticle-DNA interactions: an atomic force microscopy study.

Glyconanoparticles which present carbohydrate and amino groups motifs at their surface were produced. These particles were highly stable and soluble in aqueous solutions. The presence of the carbohydrate groups also allowed the inclusion of more strongly binding groups, without affecting solubility. The binding of a model DNA, plasmid by these nanoparticles was studied by atomic force microscopy, transmission electron microscopy, and gel electrophoresis. Significant differences between the nanoparticles based on their affinities for the DNA were found, with implications for their potential use as nonviral gene delivery agents.     

Lipid damage in farmed rainbow trout (Oncorhynchus mykiss) after slaughtering and chilled storage

The flow ice system including ozone (OFI condition) was tested for slaughtering and storage (up to 16 days) of farmed rainbow trout (Oncorhynchus mykiss). Lipid damage analyses were carried out and compared to sensory acceptance and instrumental colour changes. Comparison to individuals processed with the flow ice system in the absence of ozone (FI condition) was undertaken. Rainbow trout slaughtered and chilled under FI and OFI conditions showed a low lipid damage development, according to lipid oxidation and hydrolysis events and lipid composition (polyunsaturated fatty acids, phospholipids and endogenous antioxidants) changes. Additionally, both icing conditions led to largely good quality and shelf life times and to the absence of changes in colour properties. It is concluded that flow ice as such, or including the presence of ozone, can be considered as ideal strategy to be employed as slaughtering and storage system during the commercialisation of the actual farmed species. The ozone presence has shown some profitable effects as leading to an extended shelf life time by quality retention of several sensory parameters; in contrast, some negligible negative effects could be observed on the secondary and tertiary lipid oxidation development. However, the oxidation values reached by individuals kept under OFI conditions cannot be considered as particularly high.